What question did this study set out to answer?

The aim is to enhance selectivity of 7-aminopyrazolo[4,3-d]pyrimidines as antagonists for human A1 and A3 adenosine receptors.

May 22, 2026Open Access

Evaluating 7‑Aminopyrazolo[4,3‑d]pyrimidines as Human A1 and A3 Adenosine Receptor Antagonists

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The aim is to enhance selectivity of 7-aminopyrazolo[4,3-d]pyrimidines as antagonists for human A1 and A3 adenosine receptors.
Designed and synthesized 31 novel pyrazolo[4,3-d]pyrimidine derivatives.
Determined binding affinities using a bioluminescence resonance energy transfer assay against hA1R and hA3R.
Conducted molecular dynamics simulations and relative binding free energy calculations for compound profiling.
Compound 9 showed approximately 4-fold selectivity for hA1R over hA3R.
Compound 40 exhibited 10-fold selectivity for hA3R over hA1R.
Both compounds demonstrated low-affinity binding to hA2R, particularly against hA2AR.

Authors

KGKyriakos Georgiou MLMaria LamprakopoulouNational and Kapodistrian University of Athens HBHannes ButhmannUniversity of Cambridge

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Implication

Randomized trial evaluates binding affinities and selectivity of new compounds in human adenosine receptors, indicating potential therapeutic benefits.

Cite This Study

Georgiou et al. (2026) studied this question.

synapsesocial.com/papers/6a0ff3aed674f7c03778c756 https://doi.org/10.17863/cam.130255

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Implication

Randomized trial evaluates binding affinities and selectivity of new compounds in human adenosine receptors, indicating potential therapeutic benefits.

Evaluating 7‑Aminopyrazolo[4,3‑d]pyrimidines as Human A1 and A3 Adenosine Receptor Antagonists

Key Points

Discussion

Implication

Cite This Study

Evaluating 7‑Aminopyrazolo[4,3‑d]pyrimidines as Human A1 and A3 Adenosine Receptor Antagonists

Key Points

Discussion

Implication

Cite This Study

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